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[CAS NO. 1001264-89-6] Ipatasertib

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Catalog:	HY-15186
Brand:	MCE
CAS:	1001264-89-6

Overview

MDL	MFCD22124514
Molecular Weight	458.00
Molecular Formula	C24H32ClN5O2
SMILES	ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1

For research use only. We do not sell to patients.

26 Publications Citing Use of MCE

[1]Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.
[2]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
[3]Mol Cell. 2020 Sep 17;79(6):1008-1023.e4.
[4]Mol Cell. 2019 Jan 3;73(1):22-35.e6.
[5]Cancer Res. 2021 Mar 8;canres.3232.2020.
[6]Cell Rep. 2021 Feb 16;34(7):108744.
[7]EMBO Rep. 2020 Mar 4;21(3):e49129.
[8]Haematologica. 2020 Mar;105(3):661-673.
[9]Elife. 2020 Dec 7;9:e61405.
[10]Oncoimmunology. 2018 Aug 6;7(10):e1488565.
[11]Cancer Immunol Immunother. 2020 Nov;69(11):2259-2273.
[12]Int J Cancer. 2021 Apr 12.
[13]Oxid Med Cell Longev. 2021 Jan 12;2021:3010548.
[14]Biochem Pharmacol. 2020 Oct;180:114145.
[15]Skelet Muscle. 2021 Mar 15;11(1):6.
[16]Life Sci. 2021 Apr 19;277:119520.
[17]Life Sci. 2020 Sep 1;256:117955.
[18]Oncol Rep. 2018 Aug;40(2):635-646.
[19]Oncotargets Ther. 2020 Aug 18;13:8197-8208.
[20]Biomed Chromatogr. 2020 Oct;34(10):e4923.
[21]Biomed Chromatogr. 2020 Oct;34(10):e4920.
[22]Patent. US20220313694A1.
[23]Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140.
[24]Department of Laboratory Medicine, Laboratory of Hematology of the Radboudumc and Radboud Institute for Molecular Life Sciences in Nijmegen, The Netherlands.2019 Oct.
[25]Oncotarget. 2016 May 17;7(20):29131-42.
[26]Harvard Medical School LINCS LIBRARY

Summary

Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC ₅₀ s of 5, 18 and 8 nM for Akt1 , Akt2 and Akt3 , respectively.

IC50 & Target

Akt1

5 nM (IC ₅₀ )

Akt3

8 nM (IC ₅₀ )

Akt2

18 nM (IC ₅₀ )

PKA

3100 nM (IC ₅₀ )

In Vitro

Ipatasertib (GDC-0068) shows more than 600 and more than 100-fold selectivity for Akt1 in IC ₅₀ against the closely related kinases PKA and p70S6K, respectively. When tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members, GDC-0068 inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K). IC ₅₀ s measured for these 3 kinases are 98, 69, and 860 nM, respectively. Thus, with the exception of PKG1 (relative to which Ipatasertib (GDC-0068) is >10-fold more selective for Akt1), Ipatasertib (GDC-0068) displays a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib (GDC-0068) is investigated in 3 xenograft models that showed dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC ₅₀ of GDC-0068 in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ipatasertib (GDC-0068) is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib (GDC-0068) in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib (GDC-0068) is combined with NSC 241240. The combination of Ipatasertib (GDC-0068) with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04650581	Canadian Cancer Trials Group\|Hoffmann-La Roche	Breast Cancer	December 1, 2020	Phase 3
NCT04467801	Jun Zhang, MD, PhD\|University of Iowa\|University of Kentucky\|University of Kansas Medical Center	NSCLC Stage IV\|NSCLC Stage IIIB	September 14, 2021	Phase 2
NCT01485861	Genentech, Inc.	Prostate Cancer	January 11, 2012	Phase 1\|Phase 2
NCT04253561	SOLTI Breast Cancer Research Group\|Roche Pharma AG	Metastatic Breast Cancer	February 25, 2020	Phase 1
NCT04561817	Icahn School of Medicine at Mount Sinai	Ovarian Neoplasms	October 1, 2020	Phase 2
NCT03673787	Institute of Cancer Research, United Kingdom\|Hoffmann-La Roche	Solid Tumor\|Glioblastoma Multiforme\|Prostate Cancer Metastatic	August 13, 2018	Phase 1\|Phase 2
NCT04931342	Hoffmann-La Roche\|GOG Foundation\|European Network of Gynaecological Oncological Trial Groups (ENGOT)	Ovarian Cancer	October 7, 2021	Phase 2
NCT03337724	Hoffmann-La Roche	Breast Cancer	January 6, 2018	Phase 3
NCT04589845	Hoffmann-La Roche	Solid Tumors	January 18, 2021	Phase 2
NCT03853707	City of Hope Medical Center\|National Cancer Institute (NCI)	Anatomic Stage IV Breast Cancer AJCC v8\|Metastatic Triple-Negative Breast Carcinoma\|Prognostic Stage IV Breast Cancer AJCC v8	March 4, 2019	Phase 1\|Phase 2
NCT04464174	MedSIR\|Hoffmann-La Roche	Triple Negative Breast Cancer	October 8, 2020	Phase 2
NCT05276973	National Cancer Institute (NCI)\|NRG Oncology	Fallopian Tube Endometrioid Adenocarcinoma\|Fallopian Tube High Grade Serous Adenocarcinoma\|Ovarian Endometrioid Adenocarcinoma\|Ovarian High Grade Serous Adenocarcinoma\|Primary Peritoneal Endometrioid Adenocarcinoma\|Primary Peritoneal High Grade Serous Adenocarcinoma\|Stage III Fallopian Tube Cancer AJCC v8\|Stage III Ovarian Cancer AJCC v8\|Stage III Primary Peritoneal Cancer AJCC v8\|Stage IV Fallopian Tube Cancer AJCC v8\|Stage IV Ovarian Cancer AJCC v8\|Stage IV Primary Peritoneal Cancer AJCC v8\|Unresectable Fallopian Tube Endometrioid Adenocarcinoma\|Unresectable Fallopian Tube High Grade Serous Adenocarcinoma\|Unresectable Ovarian Endometrioid Adenocarcinoma\|Unresectable Ovarian High Grade Serous Adenocarcinoma\|Unresectable Primary Peritoneal Endometrioid Adenocarcinoma\|Unresectable Primary Peritoneal High Grade Serous Adenocarcinoma	June 27, 2022	Phase 1
NCT03072238	Hoffmann-La Roche	Metastatic Prostate Cancer	June 30, 2017	Phase 3
NCT01362374	Genentech, Inc.	Neoplasms	July 11, 2011	Phase 1
NCT04486352	Alliance Foundation Trials, LLC.\|Genentech, Inc.\|Foundation Medicine\|Pfizer	Endometrial Cancer	October 20, 2021	Phase 1\|Phase 2
NCT04591431	Fondazione per la Medicina Personalizzata	Breast Cancer\|Gastrointestinal Cancer\|Non Small Cell Lung Cancer\|Other Cancer	October 7, 2020	Phase 2
NCT01562275	Genentech, Inc.	Neoplasms	April 2012	Phase 1
NCT05498896	Queen Mary University of London\|Westdeutsche Studiengruppe GmbH (WSG)\|MedSIR\|Hoffmann-La Roche	Triple Negative Breast Cancer	December 19, 2018	Phase 2
NCT05564377	National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Locally Advanced Malignant Solid Neoplasm	December 9, 2022	Phase 2
NCT02063581	Genentech, Inc.	Healthy Volunteer	February 2014	Phase 1
NCT04920708	Royal Marsden NHS Foundation Trust\|Pfizer\|Hoffmann-La Roche	Metastatic Breast Cancer\|ER&addition; Breast Cancer\|Advanced Breast Cancer	August 2021	Phase 2
NCT05332561	German Cancer Research Center	Early-stage Breast Cancer	December 2022	Phase 2
NCT03222310	Hoffmann-La Roche	Healthy Volunteers	July 18, 2017	Phase 1
NCT03341884	Genentech, Inc.	Hepatic Insufficiency	November 9, 2017	Phase 1
NCT05172258	National Cancer Institute (NCI)	Head and Neck Squamous Cell Carcinoma\|Metastatic Head and Neck Squamous Cell Carcinoma\|Metastatic Hypopharyngeal Squamous Cell Carcinoma\|Metastatic Laryngeal Squamous Cell Carcinoma\|Metastatic Oral Cavity Squamous Cell Carcinoma\|Metastatic Oropharyngeal Squamous Cell Carcinoma\|Pathologic Stage IV HPV-Mediated (p16-Positive) Oropharyngeal Carcinoma AJCC v8\|Recurrent Head and Neck Squamous Cell Carcinoma\|Recurrent Hypopharyngeal Squamous Cell Carcinoma\|Recurrent Laryngeal Squamous Cell Carcinoma\|Recurrent Oral Cavity Squamous Cell Carcinoma\|Recurrent Oropharyngeal Squamous Cell Carcinoma\|Stage IV Hypopharyngeal Carcinoma AJCC v8\|Stage IV Laryngeal Cancer AJCC v8\|Stage IV Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage IVA Hypopharyngeal Carcinoma AJCC v8\|Stage IVA Laryngeal Cancer AJCC v8\|Stage IVA Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage IVB Hypopharyngeal Carcinoma AJCC v8\|Stage IVB Laryngeal Cancer AJCC v8\|Stage IVB Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage IVC Hypopharyngeal Carcinoma AJCC v8\|Stage IVC Laryngeal Cancer AJCC v8\|Stage IVC Oropharyngeal (p16-Negative) Carcinoma AJCC v8	April 15, 2022	Phase 2
NCT03959891	Massachusetts General Hospital\|Genentech, Inc.	Breast Cancer	May 30, 2019	Phase 1
NCT03498521	Hoffmann-La Roche\|Foundation Medicine, Inc.	Cancer of Unknown Primary Site	July 10, 2018	Phase 2
NCT04632992	Genentech, Inc.	Advanced Unresectable or Metastatic Solid Malignancy	January 13, 2021	Phase 2
NCT03280563	Hoffmann-La Roche	Breast Neoplasms	December 26, 2017	Phase 1\|Phase 2
NCT03800836	Hoffmann-La Roche	Breast Cancer	February 13, 2018	Phase 1
NCT03337698	Hoffmann-La Roche	Carcinoma, Non-Small-Cell Lung	January 2, 2018	Phase 1\|Phase 2
NCT02536391	Genentech, Inc.	Cancer	October 2015	Phase 1
NCT02301988	Genentech, Inc.\|SOLTI Breast Cancer Research Group	Breast Cancer	February 17, 2015	Phase 2
NCT01896531	Genentech, Inc.	Gastric Cancer	August 14, 2013	Phase 2
NCT02162719	Genentech, Inc.	Breast Neoplasms	August 19, 2014	Phase 2
NCT02465060	National Cancer Institute (NCI)	Advanced Malignant Solid Neoplasm\|Bladder Carcinoma\|Breast Carcinoma\|Cervical Carcinoma\|Colon Carcinoma\|Colorectal Carcinoma\|Endometrial Carcinoma\|Esophageal Carcinoma\|Gastric Carcinoma\|Glioma\|Head and Neck Carcinoma\|Kidney Carcinoma\|Liver and Intrahepatic Bile Duct Carcinoma\|Lung Carcinoma\|Lymphoma\|Malignant Uterine Neoplasm\|Melanoma\|Ovarian Carcinoma\|Pancreatic Carcinoma\|Plasma Cell Myeloma\|Prostate Carcinoma\|Rectal Carcinoma\|Recurrent Bladder Carcinoma\|Recurrent Breast Carcinoma\|Recurrent Cervical Carcinoma\|Recurrent Colon Carcinoma\|Recurrent Colorectal Carcinoma\|Recurrent Esophageal Carcinoma\|Recurrent Gastric Carcinoma\|Recurrent Glioma\|Recurrent Head and Neck Carcinoma\|Recurrent Liver Carcinoma\|Recurrent Lung Carcinoma\|Recurrent Lymphoma\|Recurrent Malignant Solid Neoplasm\|Recurrent Melanoma\|Recurrent Ovarian Carcinoma\|Recurrent Pancreatic Carcinoma\|Recurrent Plasma Cell Myeloma\|Recurrent Prostate Carcinoma\|Recurrent Rectal Carcinoma\|Recurrent Skin Carcinoma\|Recurrent Thyroid Gland Carcinoma\|Recurrent Uterine Corpus Cancer\|Refractory Lymphoma\|Refractory Malignant Solid Neoplasm\|Refractory Plasma Cell Myeloma\|Skin Carcinoma\|Thyroid Gland Carcinoma\|Uterine Corpus Cancer	August 12, 2015	Phase 2
NCT04739202	Hospices Civils de Lyon	Gastric Adenocarcinoma\|Metastatic Gastric Cancer\|Metastatic Adenocarcinoma\|Advanced Gastric Carcinoma	March 19, 2021	Phase 2
NCT04177108	Hoffmann-La Roche	Triple-Negative Breast Cancer	November 25, 2019	Phase 3
NCT04551521	German Cancer Research Center	Metastatic or Locally Advanced Malignancies	October 12, 2021	Phase 2
NCT01090960	Genentech, Inc.	Solid Cancers	March 2010	Phase 1
NCT03424005	Hoffmann-La Roche\|Seagen Inc.\|Gilead Sciences	Triple Negative Breast Cancer	April 2, 2018	Phase 1\|Phase 2
NCT04341259	Hoffmann-La Roche	Solid Tumors	November 3, 2020	Phase 1
NCT03840200	Hoffmann-La Roche	Breast Cancer\|Prostate Cancer\|Ovarian Cancer	June 11, 2019	Phase 1
NCT05538897	National Cancer Institute (NCI)	FIGO Grade 1 Endometrial Endometrioid Adenocarcinoma\|FIGO Grade 2 Endometrial Endometrioid Adenocarcinoma\|Metastatic Endometrial Endometrioid Adenocarcinoma\|Recurrent Endometrial Endometrioid Adenocarcinoma\|Stage IV Uterine Corpus Cancer AJCC v8	January 13, 2023	Phase 1\|Phase 2
NCT05180006	Gustave Roussy, Cancer Campus, Grand Paris\|Hoffmann-La Roche	Breast Cancer	February 24, 2022	Phase 2
NCT04802759	Hoffmann-La Roche	Inoperable, Locally Advanced or Metastatic, ER-positive Breast Cancer	June 20, 2021	Phase 1\|Phase 2
NCT03385655	Canadian Cancer Trials Group\|Canadian Cancer Clinical Trials Network\|BC Cancer Foundation	Prostate Cancer	December 12, 2017	Phase 2
NCT05554380	National Cancer Institute (NCI)	Locally Advanced Malignant Solid Neoplasm\|Metastatic Malignant Solid Neoplasm\|Unresectable Malignant Solid Neoplasm	December 9, 2022	Phase 2
NCT04404140	Hoffmann-La Roche	Castration-Resistant Prostatic Cancer	July 9, 2020	Phase 1
NCT03395899	Queen Mary University of London\|Kliniken Essen-Mitte\|MedSIR\|Asan Medical Center\|Hoffmann-La Roche	Breast Cancer\|Estrogen Receptor-positive Breast Cancer	December 21, 2017	Phase 2
NCT04060862	Hoffmann-La Roche	Breast Cancer	November 15, 2019	Phase 3
NCT04737109	David VanderWeele\|Big Ten Cancer Research Consortium	Castrate Resistant Prostate Cancer	July 13, 2021	Phase 1\|Phase 2
NCT05172245	National Cancer Institute (NCI)	Head and Neck Carcinoma of Unknown Primary\|Locally Advanced Head and Neck Squamous Cell Carcinoma\|Locally Advanced Hypopharyngeal Squamous Cell Carcinoma\|Locally Advanced Laryngeal Squamous Cell Carcinoma\|Locally Advanced Nasal Cavity Squamous Cell Carcinoma\|Locally Advanced Oral Cavity Squamous Cell Carcinoma\|Locally Advanced Oropharyngeal Squamous Cell Carcinoma\|Locally Advanced Paranasal Sinus Squamous Cell Carcinoma\|Locally Advanced Sinonasal Squamous Cell Carcinoma\|Maxillary Sinus Squamous Cell Carcinoma\|Stage III Hypopharyngeal Carcinoma AJCC v8\|Stage III Laryngeal Cancer AJCC v8\|Stage III Lip and Oral Cavity Cancer AJCC v8\|Stage III Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage III Sinonasal Cancer AJCC v8\|Stage IVA Hypopharyngeal Carcinoma AJCC v8\|Stage IVA Laryngeal Cancer AJCC v8\|Stage IVA Lip and Oral Cavity Cancer AJCC v8\|Stage IVA Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage IVA Sinonasal Cancer AJCC v8\|Stage IVB Hypopharyngeal Carcinoma AJCC v8\|Stage IVB Laryngeal Cancer AJCC v8\|Stage IVB Lip and Oral Cavity Cancer AJCC v8\|Stage IVB Oropharyngeal (p16-Negative) Carcinoma AJCC v8\|Stage IVB Sinonasal Cancer AJCC v8	April 12, 2022	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 220 mg/mL ( 480.35 mM ; Need ultrasonic)

H ₂ O : 3.57 mg/mL ( 7.79 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1834 mL	10.9170 mL	21.8341 mL
5 mM	0.4367 mL	2.1834 mL	4.3668 mL
10 mM	0.2183 mL	1.0917 mL	2.1834 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 0.5% MC >> 0.5% Tween-80

Solubility: 10 mg/mL (21.83 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.
[2] Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

Synonyms

1-Propanone, 2-(4-chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-, (2S)-

(2S)-2-(4-Chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone

GDC 0068

Ipatasertib

RG 7440

RG7440

RG-7440

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